[HTML][HTML] Targeted protein degradation: current molecular targets, localization, and strategies

D Pliatsika, C Blatter, R Riedl - Drug Discovery Today, 2024 - Elsevier
Targeted protein degradation (TPD) has revolutionized drug discovery by selectively
eliminating specific proteins within and outside the cellular context. Over the past two …

An updated patent review of BRD4 degraders

Z Ma, C Zhang, AA Bolinger, J Zhou - Expert Opinion on …, 2024 - Taylor & Francis
Introduction Bromodomain-containing protein 4 (BRD4), an important epigenetic reader, is
closely associated with the pathogenesis and development of many diseases, including …

Heat Shock Protein 90 Interactome-Mediated Proteolysis Targeting Chimera (HIM-PROTAC) Degrading Glutathione Peroxidase 4 to Trigger Ferroptosis

J Dong, F Ma, M Cai, F Cao, H Li, H Liang… - Journal of Medicinal …, 2024 - ACS Publications
Targeted protein degradation (TPD) is an emerging therapeutic paradigm aimed at
eliminating the disease-causing protein with aberrant expression. Herein, we report a new …

Conformational diversity and protein–protein interfaces in drug repurposing in Ras signaling pathway

AZ Sayin, Z Abali, S Senyuz, F Cankara, A Gursoy… - Scientific Reports, 2024 - nature.com
We focus on drug repurposing in the Ras signaling pathway, considering structural
similarities of protein–protein interfaces. The interfaces formed by physically interacting …

Targeted Degradation of Protein Kinase A via a Stapled Peptide PROTAC

MK Whittaker, GN Bendzunas, M Shirani… - ACS Chemical …, 2024 - ACS Publications
Proteolysis-targeting chimeras (PROTACs) are bifunctional molecules that bind and recruit
an E3 ubiquitin ligase to a targeted protein of interest, often through the utilization of a small …

Research progress of PROTACs for neurodegenerative diseases therapy

Z Cai, Z Yang, H Li, Y Fang - Bioorganic Chemistry, 2024 - Elsevier
Neurodegenerative diseases (NDD) are characterized by the gradual deterioration of
neuronal function and integrity, resulting in an overall decline in brain function. The existing …

New implications for prion diseases therapy and prophylaxis

F Liu, W Lü, L Liu - Frontiers in Molecular Neuroscience, 2024 - frontiersin.org
Prion diseases are rare, fatal, progressive neurodegenerative disorders that affect both
animal and human. Human prion diseases mainly present as Creutzfeldt-Jakob disease …

Targeting EGFR with molecular degraders as a promising strategy to overcome resistance to EGFR inhibitors

Q Wang, Y Zhu, J Pei - Future Medicinal Chemistry, 2024 - Taylor & Francis
Abnormal activation of EGFR is often associated with various malignant tumors, making it an
important target for antitumor therapy. However, traditional targeted inhibitors have several …

Molecular Glue-Mediated Targeted Protein Degradation: A Novel Strategy in Small-Molecule Drug Development

X Tan, Z Huang, H Pei, Z Jia, J Zheng - iScience, 2024 - cell.com
Small-molecule drugs are effective and thus most widely used. However, their applications
are limited by their reliance on active high-affinity binding sites, restricting their target …

Inhibitors to degraders: Changing paradigm in drug discovery

V Haridas, S Dutta, A Munjal, S Singh - Iscience, 2024 - cell.com
The chemical understanding of biological processes provides not only a deeper insight but
also a solution to abnormal biological functioning. Protein degradation, a natural biological …